Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

GUO Kai-xin; SHI Kuan; WEN Jun; ZHOU Ting-ting; FAN Guo-rong

doi:10.3969/j.issn.1006-0111.2012.06.006

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Generally azole antifungal drugs possessed chiral center. After administration of the racemate, the results indicated the differences in plasma concentrations and pharmacokinetic parameters between enantiomers were stereoselctive. The metabolism might be mainly responsible for the chiral pharmacikinetics of the enantiomers. The quantitation of enantiomers in biological matrix was based on the development of chiral separation techniques. In this paper, the chiral separation techniques of these agents and the advance in chiral pharmacokinetics of ketoconazole and itraconazole were reviewed, which could provide some references to the discovery of azole antifungal new agents.

Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

1. School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Medical Team, 75215 Force, Huizhou 516133, China

2. School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Medical Team, 95890 Force, Wuhan 434000, China

3. School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Shanghai Key Laboratory for Pharmaceutical Metabolite Research, Shanghai 200433, China

Received Date: 2011-05-11

Rev Recd Date: 2011-10-13

Key words:

Abstract: Generally azole antifungal drugs possessed chiral center. After administration of the racemate, the results indicated the differences in plasma concentrations and pharmacokinetic parameters between enantiomers were stereoselctive. The metabolism might be mainly responsible for the chiral pharmacikinetics of the enantiomers. The quantitation of enantiomers in biological matrix was based on the development of chiral separation techniques. In this paper, the chiral separation techniques of these agents and the advance in chiral pharmacokinetics of ketoconazole and itraconazole were reviewed, which could provide some references to the discovery of azole antifungal new agents.

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Reference (24)

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Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

doi: 10.3969/j.issn.1006-0111.2012.06.006

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